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imetelstat + paclitaxel + carboplatin
- Development stage
- Phase 1
- Lead developer
- Geron
- Modality
- Small Interfering RNA (siRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, MicroRNA (miRNA) → Small RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
This combination therapy consists of **imetelstat**, a first-in-class telomerase inhibitor, administered alongside the standard chemotherapy doublet of **paclitaxel** (a microtubule stabilizer) and **carboplatin** (a DNA cross-linking agent). Imetelstat is a 13-mer lipid-conjugated oligonucleotide that binds with high affinity to the template region of the RNA component of telomerase (hTR), acting as a competitive inhibitor of telomerase activity. The combination was primarily investigated by Geron Corporation for the treatment of advanced solid tumors, including non-small cell lung cancer (NSCLC) and breast cancer. The therapeutic rationale was based on the hypothesis that telomerase inhibition could sensitize cancer cells to the cytotoxic effects of chemotherapy and target the self-renewal capacity of cancer stem cells, potentially overcoming resistance and improving clinical outcomes in telomerase-expressing malignancies.
- Other names
- GRN163L + paclitaxel + carboplatinimetelstat sodium + paclitaxel + carboplatin
02
Targets
DNATERC (Telomerase RNA component)TUBB (Tubulin (alpha and beta subunits))
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